设计和活动评价Berberine加载的双pH和酶敏感结肠准微粒的设计和活动评估
Jingqi Sun1, Xinlong Chai1, Xiwen Zeng1
1Department of Pharmaceutics, School of Pharmacy, China Jiamusi University, Jiamusi 154007, China.
Pharmaceutics
|June 27, 2025
概括
携带柏柏林的结肠向微粒 (BBR-ES MPs) 通过减少炎症和恢复肠道微生物群,有效治疗性结肠炎 (UC). 这种新的交付系统增强了BBR.
科学领域:
- 药理学 药理学是指药理学的学科.
- 胃肠病学 胃肠病学
- 材料科学 材料科学 材料科学
背景情况:
- 性结肠炎 (UC) 是一种慢性炎症性肠病,治疗选择有限.
- 传统的口服柏柏林 (BBR) 呈现出不良的结肠输送,阻碍了其对UC的治疗潜力.
- 开发有针对性的输送系统对于提高BBR在治疗结肠炎症中的有效性至关重要.
研究的目的:
- 开发和评估一种针对结肠的微粒系统 (BBR-ES MPs),使用素 (CS) 和Eudragit S-100用于性结肠炎中增强柏柏林的输送.
- 评估BBR-ESMPs在DSS诱导的UC的小鼠模型中的治疗疗效.
- 调查BBR-ES MPs对肠道微生物群组成和多样性的影响.
主要方法:
- 装有柏柏林的基托桑纳米载体被准备并涂上Eudragit S-100以创建pH/酶双响应微粒 (MP).
- 结肠向能力通过体外释放研究得到证实.
- 治疗效果在硫酸 (DSS) 诱导的UC小鼠模型中进行了评估,评估了临床症状,结肠组织学,炎症标志物 (细胞因子,MPO) 和肠道微生物群,使用16SrRNA测序.
主要成果:
- 在UC小鼠中,BBR-ES MP显著降低了疾病活性指数 (DAI),并恢复了结肠长度 (p < 0.01).
- 用BBR-ESMPs治疗降低了促炎细胞因子 (IL-1β,IL-6,TNF-α) 的调节,并提高了抗炎IL-10的调节.
- 肠道微生物群分析显示,细菌菌群和细菌菌群的比率恢复并改善了α/β多样性,BBR-ES MPs与免费BBR相比显示出更高的疗效.
结论:
- BBR-ES MPs通过pH/酶双反应机制提供有效的结肠向药物输送.
- 开发的系统显著缓解了UC相关的炎症,并调节了肠道失生症.
- BBR-ES MPs代表了一种有前途且精确的治疗策略,用于治疗性结肠炎.
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